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公开(公告)号:US5169961A
公开(公告)日:1992-12-08
申请号:US796298
申请日:1991-11-22
IPC分类号: C07C313/08 , C07C319/14 , C07C319/24 , C07C323/22 , C07D333/56 , C07D497/08
CPC分类号: C07D497/08 , C07C313/08 , C07C319/14 , C07C319/24 , C07D333/56
摘要: A process for the production in high yield of 2-acetylbenzo[.beta.]thiophene and its alkyl and alkoxy substituted derivatives by converting a 2-halobenzaldehyde to a 2,2'-dithiobis(benzaldehyde) intermediate and reacting that intermediate successively with 2,4-pentanedione and chloroacetone in the presence of base.
摘要翻译: 通过将2-卤代苯甲醛转化为2,2'-二硫代双(苯甲醛)中间体并使该中间体依次与2,4和2二硫代双 戊二酮和氯丙酮。
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2.Process for the preparation of N-4-[(substituted phenyl)alkylheterocyclic]- N 失效
标题翻译: 制备N-4 - [(取代苯基)烷基杂环基] -N-羟基脲化合物的方法公开(公告)号:US5580989A
公开(公告)日:1996-12-03
申请号:US472448
申请日:1995-06-07
申请人: James D. Ratajczyk , Juliette K. Busse , Sanjay R. Chemburkar , Daniel A. Dickman , Yi-Yin Ku , Hemantkumar H. Patel , Ramesh R. Patel , David P. Sawick , John N. Starr , Bhadra Shelat , Harry O. Spiwek
发明人: James D. Ratajczyk , Juliette K. Busse , Sanjay R. Chemburkar , Daniel A. Dickman , Yi-Yin Ku , Hemantkumar H. Patel , Ramesh R. Patel , David P. Sawick , John N. Starr , Bhadra Shelat , Harry O. Spiwek
IPC分类号: A61K31/38 , A61K31/381 , A61P29/00 , A61P37/08 , A61P43/00 , B01J27/13 , B01J31/22 , C07D307/52 , C07D333/20 , C07D333/22 , C07D307/36
CPC分类号: C07D333/20 , C07D307/52
摘要: A process for preparing a compound of the structure I ##STR1## where A is oxygen and sulfur and R.sup.1 is selected from the group consisting of hydrogen, halogen, alkyl of one to six carbon atoms, alkoxy of one to six carbon atoms, and trifluoromethyl, and R.sup.2 is alkyl of one to four carbon atoms, comprising coupling a compound of formula II: ##STR2## where X is bromine or iodine, with an N-hydroxyurea compound of formula III: ##STR3## in the presence of a palladium catalyst followed by reaction of the product thus formed with an alkali metal isocyante.The compounds of formula I are inhibitors of the enzyme 5-lipoxygenase and are thus useful as therapeutic agents for the treatment of allergic and inflammatory disease conditions.
摘要翻译: 制备结构I I的化合物的方法,其中A是氧和硫,R 1选自氢,卤素,1至6个碳原子的烷基,1至6个碳原子的烷氧基,以及 三氟甲基,R 2为1-4个碳原子的烷基,其中包括式I化合物:其中X为溴或碘的式II化合物与式III的N-羟基脲化合物: 钯催化剂,随后将由此形成的产物与碱金属异氰酸酯反应。 式I化合物是5-脂氧合酶的抑制剂,因此可用作治疗过敏性和炎性疾病病症的治疗剂。
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公开(公告)号:US5275950A
公开(公告)日:1994-01-04
申请号:US15873
申请日:1993-02-10
申请人: Daniel A. Dickman , Bruce W. Horrom , Chi-Nung W. Hsiao , M. Robert Leanna , Hormoz Mazdiyasni , Howard E. Morton , Thomas M. Zydowsky , William R. Baker , Stephen L. Condon
发明人: Daniel A. Dickman , Bruce W. Horrom , Chi-Nung W. Hsiao , M. Robert Leanna , Hormoz Mazdiyasni , Howard E. Morton , Thomas M. Zydowsky , William R. Baker , Stephen L. Condon
IPC分类号: A61K38/00 , C07D277/28 , C07D277/46 , C07D295/26 , C07K5/065 , C12P13/04 , C07D241/04 , C12P11/00 , C12P17/12
CPC分类号: C07D277/28 , C07D295/26 , C07K5/06078 , A61K38/00
摘要: Intermediates and a process for their preparation are disclosed which are useful for the preparation of a renin inhibiting compound of the formula: ##STR1## wherein R is a nitrogen-containing heterocycle which is bonded via a nitrogen atom to the sulfonyl group, R.sub.6 is hydrogen, alkoxy, halogen or loweralkyl, R.sub.7 is loweralkyl having 2 to 7 carbon atoms, and R.sub.8 is loweralkyl, cycloalkyl, or aryl or a pharmaceutically acceptable acid addition salt thereof.
摘要翻译: 公开了中间体及其制备方法,其可用于制备下式的肾素抑制化合物:(*化学结构*)(I)其中R是通过氮原子与氮原子键合的含氮杂环 磺酰基,R6是氢,烷氧基,卤素或低级烷基,R7是具有2-7个碳原子的低级烷基,R8是低级烷基,环烷基或芳基或其药学上可接受的酸加成盐。
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公开(公告)号:US07968707B2
公开(公告)日:2011-06-28
申请号:US11679227
申请日:2007-02-27
申请人: Hing Leung Sham , Daniel W. Norbeck , Xiaoqi Chen , David A. Betebenner , Dale J. Kempf , Thomas R. Herrin , Gondi N. Kumar , Stephen L. Condon , Arthur J. Cooper , Daniel A. Dickman , Steven M. Hannick , Lawrence Kolaczkowski , Patricia A. Oliver , Daniel J. Plata , Peter J. Stengel , Eric J. Stoner , Jieh-Heh J. Tien , Jih-Hua Liu , Ketan M. Patel
发明人: Hing Leung Sham , Daniel W. Norbeck , Xiaoqi Chen , David A. Betebenner , Dale J. Kempf , Thomas R. Herrin , Gondi N. Kumar , Stephen L. Condon , Arthur J. Cooper , Daniel A. Dickman , Steven M. Hannick , Lawrence Kolaczkowski , Patricia A. Oliver , Daniel J. Plata , Peter J. Stengel , Eric J. Stoner , Jieh-Heh J. Tien , Jih-Hua Liu , Ketan M. Patel
IPC分类号: C07D219/04 , C07D291/06 , C07D243/04 , C07D265/12 , C07D413/12 , C07D239/02
CPC分类号: C07D207/27 , C07D207/404 , C07D207/408 , C07D223/10 , C07D233/32 , C07D233/42 , C07D239/10 , C07D239/22 , C07D241/08 , C07D241/18 , C07D253/06 , C07D263/22 , C07D307/20 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D417/12
摘要: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
摘要翻译: 公开了下式的化合物作为HIV蛋白酶抑制剂。 还公开了用于抑制HIV感染的方法和组合物。
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公开(公告)号:US20100234456A1
公开(公告)日:2010-09-16
申请号:US12787140
申请日:2010-05-25
申请人: Michael D. Wendt , Hong Ding , Sheela A. Thomas , Steven W. Elmore , Wang Shen , Daniel A. Dickman , David Augeri
发明人: Michael D. Wendt , Hong Ding , Sheela A. Thomas , Steven W. Elmore , Wang Shen , Daniel A. Dickman , David Augeri
IPC分类号: A61K31/255 , C07C39/24 , A61K31/055 , C07C39/04 , A61K31/05 , C07C305/22 , C07C47/52 , A61K31/11 , C07C63/00 , A61K31/192 , C07C211/44 , A61K31/135 , A61P35/00
CPC分类号: C07C311/41 , C07C63/48 , C07C63/49 , C07C65/26 , C07C65/28 , C07C205/58 , C07C229/52 , C07C229/56 , C07C233/81 , C07C311/13 , C07C311/18 , C07C311/21 , C07C311/37 , C07C311/44 , C07C323/20 , C07C323/25 , C07C323/62 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07C2603/18 , C07C2603/74 , C07D207/30 , C07D213/53 , C07D215/12 , C07D215/48 , C07D333/34
摘要: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds and methods of treating diseases during which are expressed the Mcl-1 protein are disclosed.
摘要翻译: 公开了抑制抗细胞凋亡Mcl-1蛋白活性的化合物,含有该化合物的组合物和治疗疾病的方法,其表达为Mcl-1蛋白。
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公开(公告)号:US08796451B2
公开(公告)日:2014-08-05
申请号:US13107780
申请日:2011-05-13
申请人: Daniel A. Dickman , Sanjay Chemburkar , James J. Fort , Rodger F. Henry , David Lechuga-Ballesteros , Yuping Niu , William Porter
发明人: Daniel A. Dickman , Sanjay Chemburkar , James J. Fort , Rodger F. Henry , David Lechuga-Ballesteros , Yuping Niu , William Porter
IPC分类号: C07D239/36 , C07D239/10
CPC分类号: C07D239/10 , A61K9/4866 , A61K31/00 , A61K31/513 , A61K47/10 , A61K47/44 , A61K2300/00
摘要: New crystalline forms of lopinavir are disclosed.
摘要翻译: 公开了新的结晶形式的洛匹那韦。
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公开(公告)号:US07989656B2
公开(公告)日:2011-08-02
申请号:US12787140
申请日:2010-05-25
申请人: Michael D. Wendt , Hong Ding , Sheela A. Thomas , Steven W. Elmore , Wang Shen , Daniel A. Dickman , David Augeri
发明人: Michael D. Wendt , Hong Ding , Sheela A. Thomas , Steven W. Elmore , Wang Shen , Daniel A. Dickman , David Augeri
IPC分类号: C07C63/00
CPC分类号: C07C311/41 , C07C63/48 , C07C63/49 , C07C65/26 , C07C65/28 , C07C205/58 , C07C229/52 , C07C229/56 , C07C233/81 , C07C311/13 , C07C311/18 , C07C311/21 , C07C311/37 , C07C311/44 , C07C323/20 , C07C323/25 , C07C323/62 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07C2603/18 , C07C2603/74 , C07D207/30 , C07D213/53 , C07D215/12 , C07D215/48 , C07D333/34
摘要: The present invention relates to biaryl carboxylic acid compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing these compounds and methods of treating diseases which express the Mcl-1 protein.
摘要翻译: 本发明涉及抑制抗细胞凋亡Mcl-1蛋白活性的联芳羧酸化合物,含有这些化合物的组合物和治疗表达Mcl-1蛋白的疾病的方法。
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公开(公告)号:US07504512B2
公开(公告)日:2009-03-17
申请号:US10820097
申请日:2004-04-07
申请人: David J. Augeri , Steven A. Baumeister , Milan Bruncko , Daniel A. Dickman , Hong Ding , Jurgen Dinges , Stephen W. Fesik , Philip J. Hajduk , Aaron R. Kunzer , William McClellan , David G. Nettesheim , Thorsten Oost , Andrew M. Petros , Saul H. Rosenberg , Wang Shen , Sheela A. Thomas , Xilu Wang , Michael D. Wendt
发明人: David J. Augeri , Steven A. Baumeister , Milan Bruncko , Daniel A. Dickman , Hong Ding , Jurgen Dinges , Stephen W. Fesik , Philip J. Hajduk , Aaron R. Kunzer , William McClellan , David G. Nettesheim , Thorsten Oost , Andrew M. Petros , Saul H. Rosenberg , Wang Shen , Sheela A. Thomas , Xilu Wang , Michael D. Wendt
IPC分类号: C07C211/00 , A61K31/445
CPC分类号: C07D207/27 , A61K31/18 , A61K31/4015 , A61K31/44 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/541 , C07C311/51 , C07C323/30 , C07C323/37 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/42 , C07C2603/74 , C07D203/26 , C07D207/06 , C07D209/08 , C07D209/52 , C07D209/54 , C07D211/22 , C07D211/74 , C07D213/54 , C07D213/61 , C07D213/64 , C07D213/70 , C07D213/78 , C07D215/12 , C07D221/20 , C07D231/12 , C07D235/08 , C07D235/26 , C07D239/26 , C07D249/04 , C07D263/32 , C07D263/56 , C07D263/58 , C07D277/56 , C07D277/64 , C07D295/205 , C07D295/26 , C07D317/60 , C07D333/28 , C07D333/56 , C07D333/70 , C07D417/12 , C07D451/02
摘要: N-Benzoyl arylsulfonamides having the formula are BCL-X1 inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-X1 inhibiting compositions and methods of promoting apoptosis in a mammal.
摘要翻译: 具有下式的N-苯甲酰基芳基磺酰胺是BCL-X1抑制剂,可用于促进凋亡。 还公开了BCL-X1抑制组合物和促进哺乳动物细胞凋亡的方法。
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公开(公告)号:US07279582B2
公开(公告)日:2007-10-09
申请号:US10280652
申请日:2002-10-25
申请人: Eric J. Stoner , Arthur J. Cooper , Lawrence Kolaczkowski , Ketan M. Patel , Hing Leung Sham , Daniel W. Norbeck , Xiaoqi Chen , David A. Betebenner , Thomas R. Herrin , Gondi N. Kumar , Stephen L. Condon , Daniel A. Dickman , Patricia A. Oliver , Jien-Heh J. Tien
发明人: Eric J. Stoner , Arthur J. Cooper , Lawrence Kolaczkowski , Ketan M. Patel , Hing Leung Sham , Daniel W. Norbeck , Xiaoqi Chen , David A. Betebenner , Thomas R. Herrin , Gondi N. Kumar , Stephen L. Condon , Daniel A. Dickman , Patricia A. Oliver , Jien-Heh J. Tien
IPC分类号: C07D233/32 , C07D239/10 , C07D239/12
CPC分类号: C07D207/27 , C07D207/404 , C07D207/408 , C07D223/10 , C07D233/32 , C07D233/42 , C07D239/10 , C07D239/22 , C07D241/08 , C07D241/18 , C07D253/06 , C07D263/22 , C07D307/20 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D417/12
摘要: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
摘要翻译: 公开了下式的化合物作为HIV蛋白酶抑制剂。 还公开了用于抑制HIV感染的方法和组合物。
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公开(公告)号:US06864369B2
公开(公告)日:2005-03-08
申请号:US10387175
申请日:2003-03-12
申请人: Daniel A. Dickman , Sanjay Chemburkar , James J. Fort , Rodger F. Henry , David Lechuga-Ballesteros , Yuping Niu , William Porter
发明人: Daniel A. Dickman , Sanjay Chemburkar , James J. Fort , Rodger F. Henry , David Lechuga-Ballesteros , Yuping Niu , William Porter
IPC分类号: C07D239/10
CPC分类号: C07D239/10 , A61K9/4866 , A61K31/00 , A61K31/513 , A61K47/10 , A61K47/44 , A61K2300/00
摘要: New crystalline forms of lopinavir are disclosed.
摘要翻译: 公开了新的结晶形式的洛匹那韦。
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